[HTML][HTML] Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and …
Free fatty acid receptors 2 and 3 (FFA2 and FFA3) are G protein-coupled receptors for short
chain free fatty acids (SCFAs). They respond to the same set of endogenous ligands but with …
chain free fatty acids (SCFAs). They respond to the same set of endogenous ligands but with …
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening
IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2008 - ACS Publications
The G-protein-coupled receptor free fatty acid receptor 1 (FFAR1), previously named GPR40,
is a possible novel target for the treatment of type 2 diabetes. In an attempt to identify new …
is a possible novel target for the treatment of type 2 diabetes. In an attempt to identify new …
[HTML][HTML] Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus …
…, NJ Smith, E Christiansen, IG Tikhonova… - Journal of Biological …, 2011 - ASBMB
Free fatty acid receptor 2 (FFA2; GPR43) is a G protein-coupled seven-transmembrane
receptor for short-chain fatty acids (SCFAs) that is implicated in inflammatory and metabolic …
receptor for short-chain fatty acids (SCFAs) that is implicated in inflammatory and metabolic …
[HTML][HTML] Identification of residues important for agonist recognition and activation in GPR40
CS Sum, IG Tikhonova, S Neumann, S Engel… - Journal of Biological …, 2007 - ASBMB
GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have
recently been identified as free fatty acids (FFAs). The receptor, now named FFA receptor 1…
recently been identified as free fatty acids (FFAs). The receptor, now named FFA receptor 1…
[HTML][HTML] Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor
FFA2 is a G protein-coupled receptor that responds to short chain fatty acids and has
generated interest as a therapeutic target for metabolic and inflammatory conditions. However, …
generated interest as a therapeutic target for metabolic and inflammatory conditions. However, …
Bidirectional, iterative approach to the structural delineation of the functional “chemoprint” in GPR40 for agonist recognition
IG Tikhonova, CS Sum, S Neumann… - Journal of medicinal …, 2007 - ACS Publications
GPR40, free fatty acid receptor 1 (FFAR1), is a member of the GPCR superfamily and a
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …
possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional …
[HTML][HTML] Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs
BD Hudson, E Christiansen, IG Tikhonova… - The FASEB …, 2012 - ncbi.nlm.nih.gov
When it is difficult to develop selective ligands within a family of related G-protein-coupled
receptors (GPCRs), chemically engineered receptors activated solely by synthetic ligands (…
receptors (GPCRs), chemically engineered receptors activated solely by synthetic ligands (…
[HTML][HTML] Old drug, new target: ellipticines selectively inhibit RNA polymerase I transcription
Transcription by RNA polymerase I (Pol-I) is the main driving force behind ribosome biogenesis,
a fundamental cellular process that requires the coordinated transcription of all three …
a fundamental cellular process that requires the coordinated transcription of all three …
Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator
…, C Tränkle, IG Tikhonova, DR Adams, G Milligan - Molecular …, 2011 - ASPET
Allosteric agonists are powerful tools for exploring the pharmacology of closely related G
protein-coupled receptors that have nonselective endogenous ligands, such as the short chain …
protein-coupled receptors that have nonselective endogenous ligands, such as the short chain …
β-Arrestin-dependent and-independent endosomal G protein activation by the vasopressin type 2 receptor
C Daly, AA Guseinov, H Hahn, A Wright, IG Tikhonova… - Elife, 2023 - elifesciences.org
This is an important study that contributes to our understanding of the role of beta-arrestins in
endosomal activation of the vasopressin type 2 receptors. While the use of a minigene as a …
endosomal activation of the vasopressin type 2 receptors. While the use of a minigene as a …